General
Preferred name
tolterodine
Synonyms
Tolterodine L-tartrate ()
(R)-(+)-Tolterodine ()
Detrol LA ()
PNU-200583E ()
Kabi-2234 ()
Tolterodine tartrate ()
(R)-Tolterodine L-tartrate ()
TOLTERODINE TARTRATE124937-52-6 ()
Tolterodine (tartrate) ()
(+)-Tolterodine ()
(R)-Tolterodine ()
PNU-200583 ()
Inconex XL ()
Neditol XL ()
Detrusitol XL ()
Santizor XL ()
Blerone XL ()
Tolterodina ()
KABI 2234 ()
Detrusitol ()
Efflosomyl XL ()
Preblacon XL ()
Mariosea XL ()
Tolterodine l-tartrate ()
Detrol ()
DETROL ()
P&D ID
PD009584
CAS
124937-51-5
124937-52-6
Tags
available
drug
Approved by
FDA
First approval
1998
Drug indication
Pain
Overactive bladder
Drug Status
approved
investigational
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
PRICE 29
DESCRIPTION Marketed formulations may contain tolterodine tartrate (PubChem CID 443878). (GtoPdb)
DESCRIPTION Tolterodine(PNU-200583) is a potent muscarinic receptor antagonists that show selectivity for the urinary bladder over salivary glands in vivo. ;IC50 Value:;Target: mAChR;in vitro: Carbachol-induced contractions of isolated guinea pig bladder were effectively inhibited by tolterodine (IC50 14 nM) and 5-HM (IC50 5.7 nM). The IC50 values were in the microM range and the antimuscarinic potency of tolterodine was 27, 200 and 370-485 times higher, respectively, than its potency in blocking histamine receptors, alpha-adrenoceptors and calcium channels. The active metabolite, 5-HM, was >900 times less potent at these sites than at bladder muscarinic receptors [1].;in vivo: Tolterodine was extensively metabolized in vivo [2]. In the passive-avoidance test, tolterodine at 1 or 3 mg/kg had no effect on memory; the latency to cross and percentage of animals crossing were comparable to controls. In contrast, scopolamine induced a memory deficit; the latency to cross was decreased, and the number of animals crossing was increased [3].
PRICE 31
DESCRIPTION Potent, non-selective muscarinic receptor antagonist (Tocriscreen Plus)
DESCRIPTION Tolterodine is a muscarinic receptor antagonist used to treat overactive bladder with urinary incontinence, urgency, and frequency. (Enamine Bioactive Compounds)
DESCRIPTION Tolterodine tartrate (PNU-200583E) is a potent antagonist for muscarinic receptor. It show selectivity for the urinary bladder and salivary glands in vivo. (TargetMol Bioactive Compound Library)
DESCRIPTION A muscarinic receptor antagonist. Used in the treatment of urinary incontinence. (BOC Sciences Bioactive Compounds)
DESCRIPTION Tolterodine ((R)-(+)-Tolterodine) is a novel and selective muscarinic-type receptor (mAChR) antagonist used in the treatment of detrusor instability and overactive bladder syndrome. (TargetMol Bioactive Compound Library)
Compound Sets
35
AdooQ Bioactive Compound Library
A10937
Axon Medchem Screening Library
2049
BOC Sciences Bioactive Compounds
r-tolterodine-cas-124937-51-5-item-84-452672
Cayman Chemical Bioactives
15027
ChEMBL Approved Drugs
CHEMBL1382
CHEMBL1722209
ChEMBL Drugs
CHEMBL1382
CHEMBL1722209
Concise Guide to Pharmacology 2017/18
360
Concise Guide to Pharmacology 2019/20
360
Concise Guide to Pharmacology 2021/22
360
Concise Guide to Pharmacology 2023/24
360
Drug Repurposing Hub
DrugBank
DB01036
DrugBank Approved Drugs
DB01036
DrugCentral
2705
DrugCentral Approved Drugs
2705
DrugMAP
DMSHPW8
DrugMAP Approved Drugs
DMSHPW8
Enamine Bioactive Compounds
EBC-13599
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EOS101138
EUbOPEN Chemogenomics Library
EUB0000929
Guide to Pharmacology
360
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1382
Mcule NIBR MoA Box Subset
MCULE-3517349035
MedChem Express Bioactive Compound Library
HY-90010
HY-A0024
NCATS Inxight Approved Drugs
WHE7A56U7K
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
Other bioactive compounds
Prestwick Chemical Library
ReFrame library
TargetMol Bioactive Compound Library
T0099
T23229
Tocriscreen Plus
3761
VGSC-DB
NA0132
NA0133
ZINC Tool Compounds
ZINC000000968336
External IDs
72
Properties
(calculated by RDKit )
Molecular Weight
325.24
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
1
Rotatable Bonds
7
Ring Count
2
Aromatic Ring Count
2
cLogP
5.34
TPSA
23.47
Fraction CSP3
0.45
Chiral centers
1.0
Largest ring
6.0
QED
0.74
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Target
mAChR
CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
mAChR antagonist
MOA
AChR antagonist
Muscarinic M3 Antagonists
acetylcholine receptor antagonist
Member status
virtual
Indication
urinary incontinence, urinary frequency
Pathway
Neuroscience
GPCR/G protein
Neuronal Signaling
Therapeutic Class
Antispasmodics
VGSC Target
Nav1.5
Recommended Cell Concentration
None
Source data